scholarly journals Alcohol-Supported Cu-Mediated 18F-Fluorination of Iodonium Salts under “Minimalist” Conditions

Molecules ◽  
2019 ◽  
Vol 24 (17) ◽  
pp. 3197 ◽  
Author(s):  
Victoriya V. Orlovskaya ◽  
Daniel J. Modemann ◽  
Olga F. Kuznetsova ◽  
Olga S. Fedorova ◽  
Elizaveta A. Urusova ◽  
...  
Keyword(s):  
Exchange Resin ◽  
Hybrid Methods ◽  
Clinical Diagnostics ◽  
The Novel ◽  
Iodonium Salts ◽  
Positron Emission ◽  
Pet Ct ◽  
Imaging Probes ◽  
Novel Method ◽  
Radiochemical Yields

In the era of personalized precision medicine, positron emission tomography (PET) and related hybrid methods like PET/CT and PET/MRI gain recognition as indispensable tools of clinical diagnostics. A broader implementation of these imaging modalities in clinical routine is closely dependent on the increased availability of established and emerging PET-tracers, which in turn could be accessible by the development of simple, reliable, and efficient radiolabeling procedures. A further requirement is a cGMP production of imaging probes in automated synthesis modules. Herein, a novel protocol for the efficient preparation of 18F-labeled aromatics via Cu-mediated radiofluorination of (aryl)(mesityl)iodonium salts without the need of evaporation steps is described. Labeled aromatics were prepared in high radiochemical yields simply by heating of iodonium [18F]fluorides with the Cu-mediator in methanolic DMF. The iodonium [18F]fluorides were prepared by direct elution of 18F− from an anion exchange resin with solutions of the corresponding precursors in MeOH/DMF. The practicality of the novel method was confirmed by the racemization-free production of radiolabeled fluorophenylalanines, including hitherto unknown 3-[18F]FPhe, in 22–69% isolated radiochemical yields as well as its direct implementation into a remote-controlled synthesis unit.

scholarly journals GMP-Compliant Radiosynthesis of [18F]GP1, a Novel PET Tracer for the Detection of Thrombi

2021 ◽  
Vol 14 (8) ◽  
pp. 739
Author(s):  
Verena Hugenberg ◽  
Marion Zerna ◽  
Mathias Berndt ◽  
Reinhard Zabel ◽  
Rainer Preuss ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Clinical Application ◽  
Thrombus Formation ◽  
The Novel ◽  
Reaction Conditions ◽  
Fibrinogen Receptor ◽  
Pet Tracer ◽  
Pet Ct ◽  
Chemical Purity ◽  
Radiochemical Yields

Thrombus formation and thromboembolic events play important roles in various cardiovascular pathologies. The key receptor involved in platelet aggregation is the fibrinogen receptor glycoprotein IIb/IIIa. [18F]GP1, a derivative of the GPIIb/IIIa antagonist elarofiban, is a specific 18F-labeled small-molecule radiotracer that binds with high affinity to GPIIb/IIIa receptors of activated platelets. An improved, robust and fully automated radiosynthesis of [18F]GP1 has been developed. [18F]GP1 has been synthesized with decay corrected radiochemical yields of 38 ± 6%, with a radiochemical concentration up to 1900 MBq/mL, molar activities of 952–9428 GBq/µmol and a radio-chemical purity >98%. After determination of the optimal reaction conditions, in particular for HPLC separation, adaption of the reaction conditions to PET center requirements, validation of the manufacturing process and the quality control methods, the synthesis of [18F]GP1 was successfully implemented to GMP standards and was available for clinical application. We describe the GMP-compliant synthesis of the novel radiotracer [18F]GP1. Moreover, we provide some proof-of-concept examples for clinical application in the cardiovascular field. PET/CT with the novel small-molecular radiotracer [18F]GP1 may serve as a novel highly sensitive tool for visualizing active platelet aggregation at the molecular level.

N,N,N-Trimethyl-5-[(2,3,5,6-tetrafluorophenoxy)carbonyl]pyridin-2-aminium trifluoromethanesulfonate a precursor for the synthesis of 2,3,5,6-tetrafluorophenyl 6-[18F]-fluoronicotinate

2018 ◽  
Vol 74 (5) ◽  
pp. 604-607 ◽  
Author(s):  
Ryan A. Davis ◽  
James C. Fettinger
Keyword(s):  
Second Step ◽  
Prosthetic Group ◽  
X Ray ◽  
X Ray Crystallography ◽  
Positron Emission ◽  
Imaging Probes ◽  
Group A ◽  
Radiochemical Yields ◽  
Cl Atom

The synthesis, recrystallization, and X-ray deterimination of N,N,N-trimethyl-5-[(2,3,5,6-tetrafluorophenoxy)carbonyl]pyridin-2-aminium trifluoromethanesulfonate (PyTFP-precursor), C15H13F4N2O2 +·CF3SO3 −, is described. This triflate salt precursor is required for the synthesis of 2,3,5,6-tetrafluorophenyl 6-[18F]-fluoronicotinate ([18F]FPyTFP), a prosthetic group used to radiolabel peptides for positron emission tomography (PET), as peptides are increasingly being used as PET-imaging probes in nuclear medicine. Radiolabeling of peptides is typically done using a `prosthetic group', a small synthon to which the radioisotope is attached in the first step, followed by attachment to the peptide in the second step. During the synthesis of the PyTFP-precursor, displacement of a Cl atom with trimethylamine gas and anion replacement with a triflate counter-ion is critical, as incomplete replacement would hinder radioisotopic incorporation of nucleophilic fluorine-18 and result in diminished radiochemical yields. The structural determination of the PyTFP-precursor by X-ray crystallography helped confirm the anion exchange of chloride with triflate.

Motion correction in PET/CT

2005 ◽  
Vol 44 (S 01) ◽  
pp. S46-S50 ◽  
Author(s):  
M. Dawood ◽  
N. Lang ◽  
F. Büther ◽  
M. Schäfers ◽  
O. Schober ◽  
...  
Keyword(s):  
Optical Flow ◽  
Motion Correction ◽  
Motion Vector ◽  
Emission Tomography ◽  
Cardiac Pet ◽  
Novel Approach ◽  
Positron Emission ◽  
Pet Ct ◽  
Flow Algorithm ◽  
Motion Vector Field

Summary:Motion in PET/CT leads to artifacts in the reconstructed PET images due to the different acquisition times of positron emission tomography and computed tomography. The effect of motion on cardiac PET/CT images is evaluated in this study and a novel approach for motion correction based on optical flow methods is outlined. The Lukas-Kanade optical flow algorithm is used to calculate the motion vector field on both simulated phantom data as well as measured human PET data. The motion of the myocardium is corrected by non-linear registration techniques and results are compared to uncorrected images.

A novel method for the determination of linting propensity of paper

TAPPI Journal ◽  
2012 ◽  
Vol 11 (10) ◽  
pp. 9-17
Author(s):  
ALESSANDRA GERLI ◽  
LEENDERT C. EIGENBROOD
Keyword(s):  
Ash Content ◽  
The Novel ◽  
Offset Printing ◽  
Excellent Correlation ◽  
End Conditions ◽  
Bottom Side ◽  
Novel Method ◽  
Total Fraction

A novel method was developed for the determination of linting propensity of paper based on printing with an IGT printability tester and image analysis of the printed strips. On average, the total fraction of the surface removed as lint during printing is 0.01%-0.1%. This value is lower than those reported in most laboratory printing tests, and more representative of commercial offset printing applications. Newsprint paper produced on a roll/blade former machine was evaluated for linting propensity using the novel method and also printed on a commercial coldset offset press. Laboratory and commercial printing results matched well, showing that linting was higher for the bottom side of paper than for the top side, and that linting could be reduced on both sides by application of a dry-strength additive. In a second case study, varying wet-end conditions were used on a hybrid former machine to produce four paper reels, with the goal of matching the low linting propensity of the paper produced on a machine with gap former configuration. We found that the retention program, by improving fiber fines retention, substantially reduced the linting propensity of the paper produced on the hybrid former machine. The papers were also printed on a commercial coldset offset press. An excellent correlation was found between the total lint area removed from the bottom side of the paper samples during laboratory printing and lint collected on halftone areas of the first upper printing unit after 45000 copies. Finally, the method was applied to determine the linting propensity of highly filled supercalendered paper produced on a hybrid former machine. In this case, the linting propensity of the bottom side of paper correlated with its ash content.

The Potential Value of Hybrid Positron Emission Tomography/Dual-Source Computed Tomography Imaging in Coronary Bypass Surgery

2011 ◽  
Vol 14 (5) ◽  
pp. 283 ◽  
Author(s):  
Andre Plass ◽  
Maximilian Y. Emmert ◽  
Oliver Gaemperli ◽  
Hatem Alkadhi ◽  
Philipp Kaufmann ◽  
...  
Keyword(s):  
Computed Tomography ◽  
Positron Emission Tomography ◽  
Coronary Artery ◽  
Coronary Angiography ◽  
Myocardial Perfusion ◽  
Predictive Value ◽  
Bypass Surgery ◽  
Emission Tomography ◽  
Positron Emission ◽  
Pet Ct

<p><b>Background:</b> We evaluated how comprehensive assessment of coronary artery lesions and their hemodynamic relevance by means of hybrid positron emission tomography (PET) and computed tomography (CT) imaging would affect decision-making in coronary artery bypass surgery (CABG), compared with using invasive coronary angiography (ICA) alone.</p><p><b>Methods:</b> After undergoing ICA, 27 patients (21 men and 6 women; mean SD age, 66 � 10 years) planned for cardiac surgery were scheduled for myocardial perfusion stress/rest evaluation with [13N]ammonia PET and CT coronary angiography. Only ICA was available to the surgeon. Postoperatively, the performed CABG was compared with the hypothetical strategy based on hybrid PET/CT findings (regional coronary flow reserve [CFR], myocardial perfusion defects). Procedures included CABG (n = 18) alone, CABG combined with valve replacement (n = 6), and CABG combined with isolated valve replacement (n = 3). A total of 56 bypass grafts (28 venous and 28 arterial) and 66 distal anastomoses were placed.</p><p><b>Results:</b> CT evaluation showed 93% concordance (66/71) with ICA regarding significant stenoses, with sensitivity, specificity, positive predictive value, and negative predictive value of 93.1%, 98.7%, 94.4%, and 98.4%, respectively. In the PET scan, 16 patients had 1 ischemic region, and 12 patients had 1 scar region, including 5 patients who presented with mixed conditions (scar and ischemia). One patient had a completely normal myocardium. Compared with the performed surgery, PET/CT fusion evaluation showed that of the performed anastomoses, 48% had documented ischemia (with a CFR <2 in 86%), 38% were nonischemic (although a CFR value <2 was found in 78%), and 14% had scar tissue (fixed perfusion defect).</p><p><b>Conclusions:</b> Although <50% of bypasses were placed to areas with myocardial ischemia, the CFR was low in the majority of nonischemic regions, a finding that may have important prognostic relevance. PET/CT fusion imaging could potentially influence planning for CABG and provide incremental prognostic information.</p>

PET Imaging of Adenosine Receptors in Diseases

2019 ◽  
Vol 19 (16) ◽  
pp. 1445-1463 ◽  
Author(s):  
Jindian Li ◽  
Xingfang Hong ◽  
Guoquan Li ◽  
Peter S. Conti ◽  
Xianzhong Zhang ◽  
...  
Keyword(s):  
Pet Imaging ◽  
Adenosine Receptors ◽  
Neurological Diseases ◽  
G Protein Coupled Receptors ◽  
Extracellular Adenosine ◽  
Positron Emission ◽  
Imaging Probes ◽  
Pet Probes ◽  
Cancer And Inflammation ◽  
G Protein Coupled

Adenosine receptors (ARs) are a class of purinergic G-protein-coupled receptors (GPCRs). Extracellular adenosine is a pivotal regulation molecule that adjusts physiological function through the interaction with four ARs: A1R, A2AR, A2BR, and A3R. Alterations of ARs function and expression have been studied in neurological diseases (epilepsy, Alzheimer’s disease, and Parkinson’s disease), cardiovascular diseases, cancer, and inflammation and autoimmune diseases. A series of Positron Emission Tomography (PET) probes for imaging ARs have been developed. The PET imaging probes have provided valuable information for diagnosis and therapy of diseases related to alterations of ARs expression. This review presents a concise overview of various ARs-targeted radioligands for PET imaging in diseases. The most recent advances in PET imaging studies by using ARs-targeted probes are briefly summarized.

FDG-PET/CT Assessment of Pulmonary Sarcoidosis: A Guide for Internists

2018 ◽  
Vol 15 (1) ◽  
pp. 21-25 ◽  
Author(s):  
Marco Tana ◽  
Silvio di Carlo ◽  
Marcello Romano ◽  
Massimo Alessandri ◽  
Cosima Schiavone ◽  
...  
Keyword(s):  
Computed Tomography ◽  
Fdg Pet ◽  
Correct Diagnosis ◽  
Pulmonary Sarcoidosis ◽  
High Resolution Computed Tomography ◽  
Inflammatory Conditions ◽  
Positron Emission ◽  
Pet Ct ◽  
Noncaseating Granulomas ◽  
Fdg Pet Ct

Background:18F-fluorodeoxyglucose positron emission tomography integrated with computed tomography (18-F-FDG-PET/CT) is getting wide consensus in the diagnosis and staging of neoplastic disorders and represents a useful tool in the assessment of various inflammatory conditions. </P><P> Discussion: Sarcoidosis is an uncommon disease characterized by the systemic formation of noncaseating granulomas. Lungs are the sites most often affected, and investigation with high resolution computed tomography and biopsy is essential to achieve a correct diagnosis. 18-F-FDGPET/ CT is effective in the assessment of pulmonary sarcoidosis by demonstrating pulmonary and extrathoracic involvement and findings correlate well with pulmonary function in patients affected.Conclusion:This review would illustrate the usefulness and limits of 18-F-FDG-PET/CT in the assessment of pulmonary sarcoidosis.

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